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21. 发明授权

US5235097A Process for the preparation of 2,2-dimethyl-5-(2,5-dimethyl-phenoxy)-pentanoic acid, intermediates for preparing this compound and process for preparing the intermediates 失效
标题翻译：制备2,2-二甲基-5-（2,5-二甲基 - 苯氧基） - 戊酸的方法，制备该化合物的中间体及其制备方法
公开(公告)号：US5235097A
公开(公告)日：1993-08-10
申请号：US890781
申请日：1992-06-01
申请人： Zoltan Zubovics , Gabor Feher , Lajos Toldi , Gabor Kovacs , Antal Simay , Eva Kovacs nee Bozo , Imre Moravcsik , Ferenc Szederkenyi , Gyorgy Krasznai , Gyorgyi Vereczkey nee Donath , Kalman Nagy
发明人： Zoltan Zubovics , Gabor Feher , Lajos Toldi , Gabor Kovacs , Antal Simay , Eva Kovacs nee Bozo , Imre Moravcsik , Ferenc Szederkenyi , Gyorgy Krasznai , Gyorgyi Vereczkey nee Donath , Kalman Nagy
IPC分类号： C07C51/09 , C07C69/63 , C07C69/712
CPC分类号： C07C69/712 , C07C51/09 , C07C69/63
摘要： The invention relates to an improved process for the preparation of 2,2-dimethyl-5-(2,5-dimethylphenoxy)-pentanoic acid of Formula (I) ##STR1## which comprises reacting an ester of the general Formula (X) ##STR2## wherein X represents halogen and Z stands for a straight or branched chain C.sub.1-8 alkylene group optionally substituted by one or two 2,2-dimethyl-5-halopentanoyloxy group(s), wherein halo represents chlorine or bromine, and in which alkylene group one or two methylene group(s) may be optionally replaced either by hetero atom(s) or by a bivalent heterocyclic group--with an alkali salt of 2,5-dimethylphenol of Formula (II) ##STR3## or with an ester of the latter formed with a lower alkanoic acid, and hydrolizing the aryloxy-substituted ester of the general Formula (XI) thus obtained. ##STR4## Furthermore the invention relates to intermediate compounds of the general Formula (X), wherein X and Z are as stated above, and to a process for the preparation thereof.
摘要翻译：本发明涉及制备式（I）的（2,2-二甲基-5-（2,5-二甲基苯氧基） - 戊酸（I）的改进方法，其包括使通式（（X）其中X表示卤素，Z表示任选被一个或两个2,2-二甲基-5-卤代戊酰氧基取代的直链或支链C 1-8亚烷基，其中卤代表氯或溴，并且其中亚烷基一个或两个亚甲基可以任选地被杂原子或二价杂环基取代，与式（II）的2,5-二甲基苯酚的碱金属盐（II）或与低级链烷酸形成的酯，并使由此获得的通式（XI）的芳氧基取代的酯水解。（XI）此外，本发明涉及通式（X）的中间体化合物，其中X和Z如上所述，以及其制备方法。

22. 发明授权

US5155260A Process for the preparation of 2,2-dimethyl-5-(2,5-dimethyl-phenoxy)-pentanoic acid, intermediates for preparing this compound and process for preparing the intermediates 失效
标题翻译：制备2,2-二甲基-5-（2,5-二甲基 - 苯氧基） - 戊酸的方法，用于制备该化合物的中间体和制备中间体的方法
公开(公告)号：US5155260A
公开(公告)日：1992-10-13
申请号：US698081
申请日：1991-05-10
申请人： Zoltan Zubovics , Gabor Feher , Lajos Toldi , Gabor Kovacs , Antal Simay , Eva Kovacs nee Bozo , Imre Moravcsik , Ferenc Szederkenyi , Gyorgy Krasznai , Gyorgyi Vereczkey nee Donath , Kalman Nagy
发明人： Zoltan Zubovics , Gabor Feher , Lajos Toldi , Gabor Kovacs , Antal Simay , Eva Kovacs nee Bozo , Imre Moravcsik , Ferenc Szederkenyi , Gyorgy Krasznai , Gyorgyi Vereczkey nee Donath , Kalman Nagy
IPC分类号： B01J27/08 , A61K31/19 , A61K31/235 , C07B61/00 , C07C51/09 , C07C59/48 , C07C59/64 , C07C59/68 , C07C65/21 , C07C67/31 , C07C69/63 , C07C69/712 , C07C229/24 , C07D211/34
CPC分类号： C07C69/712 , C07C51/09 , C07C69/63
摘要： The invention relates to an improved process for the preparation of 2,2-dimethyl-5-(2,5-dimethylphenoxy)-pentanoic acid of Formula (I) ##STR1## which comprises reacting an ester of the general Formula (X) ##STR2## wherein X represents halogen and Z stands for a straight or branched chain C.sub.1-8 alkylene group optionally substituted by one or two 2,2-dimethyl-5-halopentanoyloxy group(s), wherein halo represents chlorine or bromine, and in which alkylene group one or two methylene group(s) may be optionally replaced either by hetero atom(s) or by a bivalent heterocyclic group--with an alkali salt of 2,5-dimethylphenol of Formula (II) ##STR3## or with an ester of the latter formed with a lower alkanoic acid, and hydrolizing the aryloxy-substituted ester of the general Formula (XI) thus obtained. Furthermore the invention relates to intermediate compounds of the general Formula (X), wherein X and Z are as stated above, and to a process for the preparation thereof.
摘要翻译：本发明涉及制备式（I）的2,2-二甲基-5-（2,5-二甲基苯氧基） - 戊酸的改进方法，其包括使通式（X）的酯与（X）其中X表示卤素，Z表示任选被一个或两个2,2-二甲基-5-卤代戊酰氧基取代的直链或支链C 1-8亚烷基，其中卤代表氯或溴，并且其中亚烷基一个或两个亚甲基可以任选被杂原子或二价杂环基取代，与式（II）的2,5-二甲基苯酚的碱金属盐（IMAGE）（ II）或与低级链烷酸形成的酯，并使由此获得的通式（XI）的芳氧基取代的酯水解。（XI）此外，本发明涉及通式（X）的中间体化合物，其中X和Z如上所述，以及其制备方法。

23. 发明授权

US4520018A 5-Substituted-4-oxo-PGI.sub.1 derivatives, PGI.sub.1 compounds of similar structure, their pharmaceutical methods and process for the preparation of said compounds 失效
标题翻译： 5-取代的-4-氧代-PGI1衍生物，具有相似结构的PGI1化合物，其制备方法和制备所述化合物的方法
公开(公告)号：US4520018A
公开(公告)日：1985-05-28
申请号：US369543
申请日：1982-04-19
申请人： Vilmos Simonidesz , Jozsef Ivanics , Geza Galambos , Agnes Papp nee Behr , Gabor Kovacs , Judit Skopal , Ildiko Szilagyi
发明人： Vilmos Simonidesz , Jozsef Ivanics , Geza Galambos , Agnes Papp nee Behr , Gabor Kovacs , Judit Skopal , Ildiko Szilagyi
IPC分类号： A61K31/557 , A61P1/04 , A61P7/02 , A61P9/08 , A61P11/08 , C07D307/935 , C07D307/937 , A61K31/335
CPC分类号： C07D307/935 , C07C321/00 , C07D307/937
摘要： New PGI.sub.1 derivatives are disclosed as well as a process for the preparation thereof, pharmaceutical compositions containing same and methods of treatment employing same. The new compounds are useful to inhibit blood platelet aggregation induced by ADF, arachidic acid, or collagen, as well as to improve blood circulation and to inhibit gastric acid secretion.
摘要翻译：公开了新的PGI1衍生物及其制备方法，含有该PGI1衍生物的药物组合物和使用其的治疗方法。新化合物可用于抑制ADF，花生酸或胶原诱导的血小板聚集，以及改善血液循环和抑制胃酸分泌。

24. 发明授权

US4438132A 4-Oxo-PGI.sub.2 compounds, their use in inhibition of thrombii and their production 失效
标题翻译： 4-Oxo-PGI2化合物，它们用于抑制血栓形成及其产生
公开(公告)号：US4438132A
公开(公告)日：1984-03-20
申请号：US368013
申请日：1982-04-13
申请人： Gaza Galambos , Vilmos Simonidesz , Istvan Szekely , Jozsef Ivanics , Krisztina Kekesi , Gabor Kovacs , Istvan Stadler , Peter Kormoczy , Karoly Horvath
发明人： Gaza Galambos , Vilmos Simonidesz , Istvan Szekely , Jozsef Ivanics , Krisztina Kekesi , Gabor Kovacs , Istvan Stadler , Peter Kormoczy , Karoly Horvath
IPC分类号： C07D307/935 , A61K31/557 , A61P1/04 , A61P7/02 , A61P9/08 , A61P9/10 , A61P9/12 , A61P11/08 , C07C405/00 , C07D307/937
CPC分类号： C07D307/937 , C07C317/00 , Y02P20/55 , Y10S514/824 , Y10S514/926 , Y10S514/927
摘要： The invention relates to a process for the preparation of novel 4-oxo-PGI.sub.2 derivatives of formula I ##STR1## where (a) compounds of formula III ##STR2## are oxidized, then the obtained 5-substituted-4-oxo-PGI.sub.1 derivatives of general formula II ##STR3## are eliminated by the splitting off of the W-H-molecule, or (b) the compounds of formula IV ##STR4## are reacted in a solvent in the presence of a catalyst with compounds of general formula V ##STR5## then the obtained compounds of formula I are transformed if desired by saponification, hydrolysis, salt formation, insertion of a protection group to another compound which belongs to the compounds of formula I, too.The pharmaceutical products of the invention can be used for the treatment of circulatory diseases, they inhibit the aggregation of blood plaques, dilate the bronchi and inhibit the secretion of gastric acid.
摘要翻译：本发明涉及一种制备式I（I）的新型4-氧代-GII 2衍生物的方法，其中（a）式III的化合物（XIIIX）被氧化，然后得到5-取代的通过分解WH分子来消除通式II（XIIX）的4-氧代-PGI1衍生物，或（b）式IV化合物（XIVX）在溶剂中在然后如果需要，通过皂化，水解，形成盐，将保护基团插入另一种属于式（I）化合物的化合物的化合物，转化所得到的式I化合物，我也。本发明的药物可用于治疗循环系统疾病，抑制血斑聚集，扩张支气管，抑制胃酸分泌。

25. 发明授权

US4304938A Process for the preparation of 3-phenoxybenzenes 失效
标题翻译： 3-苯氧基苯的制备方法
公开(公告)号：US4304938A
公开(公告)日：1981-12-08
申请号：US106102
申请日：1979-12-21
申请人： Endre Palosi , Gergely Heja , Dezso Korbonits , Pal Kiss , Csaba Gonczi , Judit Cser nee Kun , Ida Szvoboda nee Kauzel , Gabor Kovacs , Gabor Szabo , Tamas Kallay , Laszlo Ledniczky
发明人： Endre Palosi , Gergely Heja , Dezso Korbonits , Pal Kiss , Csaba Gonczi , Judit Cser nee Kun , Ida Szvoboda nee Kauzel , Gabor Kovacs , Gabor Szabo , Tamas Kallay , Laszlo Ledniczky
IPC分类号： C07C43/295 , B01J23/00 , B01J27/00 , B01J31/00 , C07B61/00 , C07C29/14 , C07C41/00 , C07C41/26 , C07C43/23 , C07C43/263 , C07C45/00 , C07C47/575 , C07C67/00 , C07C239/00 , C07C251/48 , C07C253/00 , C07C255/37 , C07C255/53 , C07C301/00 , C07C303/32 , C07C309/24 , C07D317/14 , C07D317/16 , C07D317/22 , C07C131/00
CPC分类号： C07D317/22 , C07C255/00 , C07C309/00 , C07C41/26 , C07D317/16
摘要： 3-Phenoxybenzene derivatives are prepared by a method which comprises the steps of(a) chlorinating benzaldehyde with chlorine gas in the presence of a hydrocarbon and a Lewis acid catalyst to obtain 3-chlorobenzaldehyde; (b) reacting the 3-chlorobenzaldehyde with ethylene glycol to obtain 2-(3-chlorophenyl)-1,3-dioxolane; (c) etherifying said dioxolane with an alkali phenolate to yield the intermediate 2-(3-phenoxyphenyl)-1,3-dioxolane and converting this intermediate to the corresponding aldehyde, cyanohydrin, sulfonic acid salt or oxime derivative.
摘要翻译： 3-苯氧苯衍生物通过包括以下步骤的方法制备：（a）在烃和路易斯酸催化剂的存在下用氯气氯化苯甲醛，得到3-氯苯甲醛; （b）使3-氯苯甲醛与乙二醇反应得到2-（3-氯苯基）-1,3-二氧戊环; （c）用碱性酚盐醚化所述二氧戊环，得到中间体2-（3-苯氧基苯基）-1,3-二氧戊环，并将该中间体转化成相应的醛，氰醇，磺酸盐或肟衍生物。

26. 发明授权

US4299972A Preparation of cyclopropanecarboxylic acid esters 失效
标题翻译：制备环丙烷羧酸酯
公开(公告)号：US4299972A
公开(公告)日：1981-11-10
申请号：US164902
申请日：1980-07-01
申请人： Gabor Kovacs , Istvan Szekely , Marianne Lovasz nee Gaspar , Rudolf Soos , Joszef Dukai
发明人： Gabor Kovacs , Istvan Szekely , Marianne Lovasz nee Gaspar , Rudolf Soos , Joszef Dukai
IPC分类号： A01N53/08 , A01N53/10 , C07B31/00 , C07B53/00 , C07C67/00 , C07C69/743 , C07C253/00 , C07C255/39 , C07D209/49 , C07D307/935 , C07C67/18
CPC分类号： C07C69/743
摘要： A process is disclosed for the preparation of an optically active or racemic cyclopropanecarboxylic acid of the formula (I) ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and each is lower alkyl or halogen;R is a member of a group which contains various cyclic structures as set forth in the specification,the .about. valency bond represents .alpha.- and/or .beta.-configuration;the -- valency bond represents .beta.-configuration,which comprises reacting an optically active or racemic cyclopropanecarboxylic acid of the formula (VII) ##STR2## with a dimethyl-methylidene-ammonium salt of the formula (VIII) ##STR3## wherein X is halogen or lower alkoxy andY.sup.- is a halide or lower alkylsulfate ion in an anhydrous, inert organic solvent, and sebsequently reacting a dimethyl-acloxy-methylidene-ammonium salt thus obtained with an optically active, inactive or racemic alcohol of the formulaR--OHwithout isolation, in the presence of an organic base.
摘要翻译：公开了制备式（I）的光学活性或外消旋环丙烷羧酸的方法，其中R 1和R 2相同或不同，各自为低级烷基或卤素; R是包含说明书中所列的各种环状结构的基团的成员，差异化合价键代表α-和/或β-构型; 价键表示β构型，其包括使式（VII）的光学活性或外消旋环丙烷羧酸与式（VIII）的二甲基亚甲基铵盐反应（VIII））其中X是卤素或低级烷氧基，Y-是在无水惰性有机溶剂中的卤化物或低级烷基硫酸根离子，然后使由此得到的二甲基 - 酰氧基 - 亚甲基 - 铵盐与光学活性的无活性或外消旋醇反应式R-OH不分离，在有机碱的存在下。

27. 发明授权

US4257962A Derivatives of bicyclic lactols 失效
标题翻译：双环乳糖的衍生物
公开(公告)号：US4257962A
公开(公告)日：1981-03-24
申请号：US942819
申请日：1978-09-15
申请人： Tibor Szabo , Laszlo Institoris , Gabor Kovacs , Gyula Dalmadi , Bela Koszegi , Istvan Stadler
发明人： Tibor Szabo , Laszlo Institoris , Gabor Kovacs , Gyula Dalmadi , Bela Koszegi , Istvan Stadler
IPC分类号： C07C405/00 , A61K31/34 , A61K31/343 , A61P7/02 , A61P25/02 , A61P35/00 , C07D307/935
CPC分类号： C07D307/935
摘要： Racemic or optically active compounds with antitumor activity of the formula: ##STR1## wherein X is oxygen or sulfur;R.sup.1 is hydrogen, C.sub.1 to C.sub.4 alkanoyl, benzoyl or phenyl-substituted benzoyl;R.sup.2 is hydrogen or C.sub.1 to C.sub.4 alkanoyl;R.sup.3 is C.sub.2 to C.sub.40 straight or branched chain alkyl substituted by hydroxy, epoxy, amino, C.sub.1 to C.sub.6 alkylamino, C.sub.1 to C.sub.6 dialkylamino, C.sub.1 to C.sub.6 alkanoyloxy or, C.sub.1 to C.sub.4 alkoxycarbonyl; cyclohexyl, phenyl unsubstituted or substituted by halogen, amino, C.sub.1 to C.sub.4 alkyl-substituted amino, C.sub.1 to C.sub.4 alkoxy, nitro, or hydroxy; C.sub.1 to C.sub.6 alkanoyl; allyl or phenyl-C.sub.1 to C.sub.4 alkyl unsubstituted or substituted by a C.sub.2 to C.sub.6 alkene group; or where X is sulfur R.sup.3 is as defined above or is C.sub.1 to C.sub.40 straight or branched chain alkyl; and.about. represents the exo- or endo-steric position in the ring and indicates an .alpha.- or .beta.-steric position in the side chain are disclosed.
摘要翻译：具有下式的抗肿瘤活性的外消旋或光学活性化合物：其中X是氧或硫; R1是氢，C1至C4烷酰基，苯甲酰基或苯基取代的苯甲酰基; R2是氢或C1-C4烷酰基; R3为C2至C40被羟基，环氧基，氨基，C1至C6烷基氨基，C1至C6二烷基氨基，C1至C6烷酰氧基或C1至C4烷氧基羰基取代的直链或支链烷基; 环己基，未取代或被卤素取代的苯基，氨基，C1至C4烷基取代的氨基，C1至C4烷氧基，硝基或羟基; C1至C6烷酰基; 烯丙基或未被取代或被C2至C6烯基取代的苯基-C1至C4烷基; 或其中X为硫的R 3如上所定义或为C 1至C 40直链或支链烷基; 而DIFFERENCE表示环中的外 - 或内 - 立体位置，并且表示侧链中的α或β-甾族位置。

28. 发明授权

US4149492A Remote release leash 失效
标题翻译：远程释放皮带
公开(公告)号：US4149492A
公开(公告)日：1979-04-17
申请号：US770778
申请日：1977-02-22
申请人： Gabor Kovacs
发明人： Gabor Kovacs
IPC分类号： A01K27/00 , F16G11/10
CPC分类号： A01K27/005
摘要： A remote release leash for a dog collar including a hand held actuator at one end, a latch at the other end, and a tube joining the actuator and latch. The latch includes a bolt, spring biased to the closed position. The actuator includes a plunger spring biased to the released position. A wire running through the tube joins the plunger to the bolt. A button in the actuator holds the plunger in the armed position, allowing the spring biased bolt to remain closed. Depression of the button releases the plunger for rearward translation, thereby to draw on the wire and pull the bolt open to release the dog. The independent biasing of the actuator and the latch allows multiple dog operation wherein a single actuator may control two or more latches. Furthermore, a transition piece may be provided to allow a single actuator to be used with any of a series of single, multiple, or elongated latching elements.
摘要翻译：用于狗颈的远程释放带，包括一端的手持致动器，另一端的闩锁，以及连接致动器和闩锁的管。闩锁包括螺栓，弹簧偏压到关闭位置。致动器包括偏置到释放位置的柱塞弹簧。穿过管的线将柱塞连接到螺栓。执行器中的按钮将柱塞保持在备用位置，允许弹簧偏压螺栓保持关闭。按钮的按压释放柱塞用于向后平移，从而在电线上拉动并拉开螺栓以释放狗。致动器和闩锁的独立偏置允许多个操作，其中单个致动器可以控制两个或多个闩锁。此外，可以设置过渡件以允许单个致动器与一系列单个，多个或细长的闩锁元件中的任何一个一起使用。

29. 发明申请

US20120321888A1 SPLICED CARBON FIBER TOW AND SPLICING METHOD 审中-公开
标题翻译：分离碳纤维管和分离方法
公开(公告)号：US20120321888A1
公开(公告)日：2012-12-20
申请号：US13580681
申请日：2011-02-24
申请人： Zsolt Rumy , Gabor Kovacs
发明人： Zsolt Rumy , Gabor Kovacs
IPC分类号： B65H69/06 , D01H15/00 , D01H4/02 , D01F9/12
CPC分类号： B65H69/065 , B65H2701/314 , B65H2701/37 , Y10T428/2918
摘要： A spliced fiber tow (40) having a uniform density along its entire length is provided. The spliced fiber tow is manufactured by rarefying the ends (22, 32) of the two fiber tow segments to be joined, aligning the rarefied regions (26, 36) and then applying pressurized gas to entangle the filaments in the rarefied regions. An apparatus (50) for forming the spliced fiber tow includes a pair of rarefying blades (86, 92) and an entanglement element (58).
摘要翻译：提供具有沿整个长度均匀密度的拼接纤维束（40）。接合的纤维束通过稀薄待连接的两个纤维束段的端部（22,32）而制造，使稀薄区域（26,36）对齐，然后施加加压气体以使细丝缠绕在稀薄区域中。用于形成拼接纤维丝束的装置（50）包括一对稀薄刀片（86,92）和缠结元件（58）。

30. 发明授权

US08050737B2 Method and medical apparatus for measuring pulmonary artery blood flow 有权
标题翻译：用于测量肺动脉血流量的方法和医疗设备
公开(公告)号：US08050737B2
公开(公告)日：2011-11-01
申请号：US12325317
申请日：2008-12-01
申请人： Gabor Kovacs , Horst Olschewski , Gert Reiter , Ursula Reiter , Rainer Kurt Rienmueller
发明人： Gabor Kovacs , Horst Olschewski , Gert Reiter , Ursula Reiter , Rainer Kurt Rienmueller
IPC分类号： A61B8/06 , A61B5/055
CPC分类号： A61B5/0263 , A61B5/021 , A61B5/055 , A61B5/7207 , A61B5/7289 , A61B8/06 , G06F19/00
摘要： In a method and apparatus for examination and evaluation of a blood flow in a pulmonary artery of a patient, measurement data are recorded, from which at least a part of the blood flow in the pulmonary artery is able to be re-constructed at least two-dimensionally in a plane defined by a longitudinal axis of the pulmonary artery and by an anterior-posterior direction, including at least at several diastolic points in time in the course of a heart cycle, after a closure of the pulmonary valve. The number of diastolic points for which an asymmetry in relation to the longitudinal axis of the pulmonary artery in the anterior-posterior direction exists is determined. A measure is then determined that characterizes how long, after the closure of the pulmonary valve, the aforementioned asymmetry exists.
摘要翻译：在用于检查和评价患者的肺动脉血流量的方法和装置中，记录测量数据，肺动脉中的至少一部分血流可从该测量数据重构至少两个在肺动脉瓣关闭后，在由肺动脉的纵向轴线和前后方向限定的平面中，包括至少在心脏周期过程中的至少几个舒张时间点。确定相对于前后方向肺动脉纵轴存在不对称的舒张点数。然后确定表征肺动脉瓣关闭后上述不对称性多久的度量。

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